EP3478295A4 - SYNTHESIS OF N- (HETEROARYL) -PYRROLO [3,2-D] PYRIMIDIN-2-AMINES - Google Patents
SYNTHESIS OF N- (HETEROARYL) -PYRROLO [3,2-D] PYRIMIDIN-2-AMINES Download PDFInfo
- Publication number
- EP3478295A4 EP3478295A4 EP17821293.2A EP17821293A EP3478295A4 EP 3478295 A4 EP3478295 A4 EP 3478295A4 EP 17821293 A EP17821293 A EP 17821293A EP 3478295 A4 EP3478295 A4 EP 3478295A4
- Authority
- EP
- European Patent Office
- Prior art keywords
- pyrrolo
- pyrimidin
- heteroaryl
- amines
- synthesis
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 230000015572 biosynthetic process Effects 0.000 title 1
- 238000003786 synthesis reaction Methods 0.000 title 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
- C07D487/20—Spiro-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
- C07D487/14—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201662357797P | 2016-07-01 | 2016-07-01 | |
PCT/US2017/040102 WO2018005865A1 (en) | 2016-07-01 | 2017-06-29 | Synthesis of n-(heteroaryl)-pyrrolo[3,2-d]pyrimidin-2-amines |
Publications (2)
Publication Number | Publication Date |
---|---|
EP3478295A1 EP3478295A1 (en) | 2019-05-08 |
EP3478295A4 true EP3478295A4 (en) | 2019-12-04 |
Family
ID=60786476
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP17821293.2A Pending EP3478295A4 (en) | 2016-07-01 | 2017-06-29 | SYNTHESIS OF N- (HETEROARYL) -PYRROLO [3,2-D] PYRIMIDIN-2-AMINES |
Country Status (12)
Country | Link |
---|---|
US (2) | US10865210B2 (es) |
EP (1) | EP3478295A4 (es) |
JP (1) | JP7106462B2 (es) |
KR (1) | KR102445288B1 (es) |
CN (1) | CN109789142B (es) |
AU (2) | AU2017290362B2 (es) |
CA (1) | CA3028752A1 (es) |
EA (1) | EA201990189A1 (es) |
IL (1) | IL263911B (es) |
MX (1) | MX2019000199A (es) |
NZ (1) | NZ749275A (es) |
WO (1) | WO2018005865A1 (es) |
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LT2968290T (lt) | 2013-03-15 | 2019-12-10 | G1 Therapeutics Inc | Laikina normalių ląstelių apsauga chemoterapijos metu |
WO2018005863A1 (en) | 2016-07-01 | 2018-01-04 | G1 Therapeutics, Inc. | Pyrimidine-based compounds for the treatment of cancer |
IL267795B2 (en) | 2017-01-06 | 2023-02-01 | G1 Therapeutics Inc | Combined treatment for cancer |
AU2018302179A1 (en) | 2017-07-18 | 2020-02-13 | Nuvation Bio Inc. | Heterocyclic compounds as adenosine antagonists |
BR112020000962A2 (pt) | 2017-07-18 | 2020-07-14 | Nuvation Bio Inc. | compostos de 1,8-naftiridinona e usos dos mesmos |
BR112020015431A2 (pt) | 2018-02-15 | 2020-12-08 | Nuvation Bio Inc. | Compostos heterocíclicos como inibidores de quinase |
CN108299317A (zh) * | 2018-03-20 | 2018-07-20 | 爱斯特(成都)生物制药股份有限公司 | 1,4-二氮杂螺[5,5]十一烷盐酸盐的合成方法 |
AU2019253706A1 (en) * | 2018-04-09 | 2020-11-26 | G1 Therapeutics, Inc. | Treatment of cancers having driving oncogenic mutations |
CN108840814B (zh) * | 2018-07-24 | 2021-09-24 | 南京药石科技股份有限公司 | 一种8-氧代-2,6,9-三氮杂螺[4.5]癸烷-2-羧酸叔丁酯制备方法 |
CN112839657A (zh) * | 2018-08-24 | 2021-05-25 | G1治疗公司 | 1,4-二氮杂螺[5.5]十一烷-3-酮改进的合成 |
KR20210116550A (ko) | 2019-01-18 | 2021-09-27 | 누베이션 바이오 인크. | 아데노신 길항제로서의 헤테로시클릭 화합물 |
CA3126931A1 (en) | 2019-01-18 | 2020-07-23 | Nuvation Bio Inc. | 1,8-naphthyridinone compounds and uses thereof |
KR20230012547A (ko) | 2020-05-19 | 2023-01-26 | 쥐원 쎄라퓨틱스, 인크. | 의학적 장애의 치료를 위한 시클린-의존성 키나제 억제 화합물 |
CN116157403A (zh) * | 2020-06-15 | 2023-05-23 | G1治疗公司 | 曲拉西利的形态及其制造方法 |
US10988479B1 (en) | 2020-06-15 | 2021-04-27 | G1 Therapeutics, Inc. | Morphic forms of trilaciclib and methods of manufacture thereof |
EP4225758A1 (en) | 2020-10-08 | 2023-08-16 | Teva Pharmaceuticals International GmbH | Solid state forms of trilaciclib and of trilaciclib salts |
CN113788837B (zh) * | 2021-08-02 | 2022-08-26 | 深圳湾实验室坪山生物医药研发转化中心 | Trilaciclib的合成方法 |
CN113754600A (zh) * | 2021-11-10 | 2021-12-07 | 天津敬康生物科技有限公司 | 1,4-二氮杂螺[5,5]十一烷-3-酮的制备方法 |
CN114014863B (zh) * | 2021-12-21 | 2022-11-29 | 武汉九州钰民医药科技有限公司 | 骨髓保护剂曲拉西利的制备方法 |
CN114014864B (zh) * | 2021-12-21 | 2022-11-25 | 武汉九州钰民医药科技有限公司 | 一种曲拉西利化合物的制备工艺 |
WO2023164255A1 (en) * | 2022-02-28 | 2023-08-31 | Teva Pharmaceuticals International Gmbh | Crystalline forms of trilaciclib and trilaciclib salts |
US11970403B2 (en) * | 2022-06-27 | 2024-04-30 | Saudi Arabian Oil Company | Method of zeolite synthesis including pH-modified water-soluble oxidized disulfide oil composition |
US11958751B2 (en) * | 2022-06-27 | 2024-04-16 | Saudi Arabian Oil Company | Method of synthesizing materials integrating supernatant recycle |
CN115477653B (zh) * | 2022-10-11 | 2024-04-09 | 安徽省庆云医药股份有限公司 | 一种曲拉西利关键中间体及曲拉西利的制备方法 |
WO2024116069A1 (en) | 2022-11-28 | 2024-06-06 | Assia Chemical Industries Ltd. | Novel trilaciclib intermediates, method of preparation and use thereof |
TWI842274B (zh) * | 2022-12-15 | 2024-05-11 | 中化合成生技股份有限公司 | 曲拉西利之製備方法及曲拉西利之前驅體 |
Citations (2)
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WO2002012238A2 (en) * | 2000-08-04 | 2002-02-14 | Warner-Lambert Company | 2-(4-PYRIDYL)AMINO-6-DIALKOXYPHENYL-PYRIDO[2,3-d]PYRIMIDIN-7-ONES |
US20140271466A1 (en) * | 2013-03-15 | 2014-09-18 | G1 Therapeutics, Inc. | HSPC-Sparing Treatments for RB-Positive Abnormal Cellular Proliferation |
Family Cites Families (31)
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US6506760B1 (en) * | 2000-04-14 | 2003-01-14 | Corvas International, Inc. | Substituted hydrazinyl heteroaromatic inhibitors of thrombin |
DE60322919D1 (de) * | 2002-09-11 | 2008-09-25 | Merck & Co Inc | 8-hydroxy-1-oxotetrahydropyrrolopyrazinverbindungen, die sich als inhibitoren von hiv-integrase eignen |
BRPI0406809A (pt) * | 2003-01-17 | 2005-12-27 | Warner Lambert Co | Heterociclos substituìdos de 2-aminopiridina como inibidores da proliferação celular |
ES2295963T3 (es) | 2004-01-08 | 2008-04-16 | F. Hoffmann-La Roche Ag | Derivados diaza-espiropiperidina como inhibidores del transportador 1 de glicina y transportador 2 de glicina. |
US7659300B2 (en) | 2004-09-08 | 2010-02-09 | Merck Sharp & Dohme Corp. | Monocyclic anilide spirolactam CGRP receptor antagonists |
US7696192B2 (en) | 2004-09-09 | 2010-04-13 | Merck Sharp & Dohme Corp. | Tricyclic anilide spirolactam CGRP receptor antagonists |
WO2006031610A2 (en) | 2004-09-13 | 2006-03-23 | Merck & Co., Inc. | Bicyclic anilide spirolactam cgrp receptor antagonists |
US7390798B2 (en) | 2004-09-13 | 2008-06-24 | Merck & Co., Inc. | Carboxamide spirolactam CGRP receptor antagonists |
US20060142312A1 (en) * | 2004-12-23 | 2006-06-29 | Pfizer Inc | C6-aryl and heteroaryl substituted pyrido[2,3-D] pyrimidin-7-ones |
US7851464B2 (en) | 2005-11-18 | 2010-12-14 | Merck Sharp & Dohme Corp. | Spirolactam aryl CGRP receptor antagonists |
EP2091533B1 (en) | 2006-12-08 | 2012-11-28 | Merck Sharp & Dohme Corp. | Constrained spirocyclic compounds as cgrp receptor antagonists |
US8153393B2 (en) | 2007-03-02 | 2012-04-10 | University Of Massachusetts | Spirolactam targeting compounds and related compounds |
JP2011518216A (ja) * | 2008-04-22 | 2011-06-23 | アストラゼネカ アクチボラグ | 置換ピリミジン−5−カルボキサミド |
GEP20135785B (en) | 2008-08-22 | 2013-03-11 | Novartis Ag | Pyrrolopyrimidine compounds as cdk inhibitors |
SI2632467T1 (sl) | 2010-10-25 | 2016-10-28 | G1 Therapeutics, Inc. | Inhibitorji CDK |
US8691830B2 (en) | 2010-10-25 | 2014-04-08 | G1 Therapeutics, Inc. | CDK inhibitors |
US8829102B2 (en) | 2010-10-27 | 2014-09-09 | Cabot Corporation | High loading carbon black masterbatch for pressure pipe applications |
EP2831080B1 (en) | 2012-03-29 | 2017-03-15 | Francis Xavier Tavares | Lactam kinase inhibitors |
WO2013163239A1 (en) | 2012-04-26 | 2013-10-31 | Francis Xavier Tavares | Synthesis of lactams |
US9227972B2 (en) | 2012-05-09 | 2016-01-05 | Merck Sharp & Dohme Corp. | Aliphatic spirolactam CGRP receptor antagonists |
WO2014144596A2 (en) | 2013-03-15 | 2014-09-18 | G1 Therapeutics, Inc. | Transient protection of hematopoietic stem and progenitor cells against ionizing radiation |
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SG11201906427QA (en) | 2017-01-23 | 2019-08-27 | Pfizer | Heterocyclic spiro compounds as magl inhibitors |
-
2017
- 2017-06-29 JP JP2018569090A patent/JP7106462B2/ja active Active
- 2017-06-29 NZ NZ749275A patent/NZ749275A/en unknown
- 2017-06-29 EP EP17821293.2A patent/EP3478295A4/en active Pending
- 2017-06-29 CN CN201780041253.5A patent/CN109789142B/zh active Active
- 2017-06-29 MX MX2019000199A patent/MX2019000199A/es unknown
- 2017-06-29 KR KR1020197002844A patent/KR102445288B1/ko active IP Right Grant
- 2017-06-29 EA EA201990189A patent/EA201990189A1/ru unknown
- 2017-06-29 AU AU2017290362A patent/AU2017290362B2/en active Active
- 2017-06-29 WO PCT/US2017/040102 patent/WO2018005865A1/en unknown
- 2017-06-29 CA CA3028752A patent/CA3028752A1/en active Pending
-
2018
- 2018-12-21 US US16/230,381 patent/US10865210B2/en active Active
- 2018-12-23 IL IL263911A patent/IL263911B/en unknown
-
2020
- 2020-12-14 US US17/121,392 patent/US11629150B2/en active Active
-
2021
- 2021-11-03 AU AU2021261879A patent/AU2021261879B2/en active Active
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2002012238A2 (en) * | 2000-08-04 | 2002-02-14 | Warner-Lambert Company | 2-(4-PYRIDYL)AMINO-6-DIALKOXYPHENYL-PYRIDO[2,3-d]PYRIMIDIN-7-ONES |
US20140271466A1 (en) * | 2013-03-15 | 2014-09-18 | G1 Therapeutics, Inc. | HSPC-Sparing Treatments for RB-Positive Abnormal Cellular Proliferation |
Non-Patent Citations (3)
Title |
---|
HARISH RAJAK ET AL: "2,5-Disubstituted-1,3,4-oxadiazoles/thiadiazole as surface recognition moiety: Design and synthesis of novel hydroxamic acid based histone deacetylase inhibitors", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, PERGAMON, AMSTERDAM, NL, vol. 21, no. 19, 3 August 2011 (2011-08-03), pages 5735 - 5738, XP028286354, ISSN: 0960-894X, [retrieved on 20110808], DOI: 10.1016/J.BMCL.2011.08.022 * |
HARISH RAJAK: "Supplementary material", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS VOLUME 21, ISSUE 19, 1 OCTOBER 2011, PAGES 5735-5738, 1 January 2011 (2011-01-01), pages 1 - 14, XP055635714, Retrieved from the Internet <URL:https://www.sciencedirect.com/science/article/pii/S0960894X11011073?via%3Dihub> [retrieved on 20191024] * |
See also references of WO2018005865A1 * |
Also Published As
Publication number | Publication date |
---|---|
JP2019520380A (ja) | 2019-07-18 |
JP7106462B2 (ja) | 2022-07-26 |
KR102445288B1 (ko) | 2022-09-19 |
US20210122755A1 (en) | 2021-04-29 |
IL263911A (en) | 2019-01-31 |
AU2021261879B2 (en) | 2024-01-04 |
US11629150B2 (en) | 2023-04-18 |
US20190135820A1 (en) | 2019-05-09 |
RU2019102643A (ru) | 2020-08-03 |
BR112018077155A2 (pt) | 2019-04-02 |
MX2019000199A (es) | 2019-09-23 |
AU2021261879A1 (en) | 2021-12-02 |
EA201990189A1 (ru) | 2019-06-28 |
IL263911B (en) | 2021-10-31 |
WO2018005865A1 (en) | 2018-01-04 |
KR20190025651A (ko) | 2019-03-11 |
CN109789142B (zh) | 2022-08-23 |
EP3478295A1 (en) | 2019-05-08 |
RU2019102643A3 (es) | 2020-08-21 |
AU2017290362A1 (en) | 2019-01-17 |
NZ749275A (en) | 2023-06-30 |
US10865210B2 (en) | 2020-12-15 |
CA3028752A1 (en) | 2018-01-04 |
AU2017290362B2 (en) | 2021-08-05 |
CN109789142A (zh) | 2019-05-21 |
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